CAS 170449-18-0|AG 1478 hydrochloride
Introduction：Basic information about CAS 170449-18-0|AG 1478 hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | AG 1478 hydrochloride | ||
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| CAS Number | 170449-18-0 | Molecular Weight | 352.215 |
| Density | 1.337g/cm3 | Boiling Point | 458.5ºC at 760mmHg |
| Molecular Formula | C16H15Cl2N3O2 | Melting Point | / |
| MSDS | / | Flash Point | 231.1ºC |
Names
| Name | N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride |
|---|---|
| Synonym | More Synonyms |
AG 1478 hydrochloride BiologicalActivity
| Description | AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV)[1][2][3][4]. |
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| Related Catalog | Signaling Pathways >>Anti-infection >>Influenza VirusResearch Areas >>CancerSignaling Pathways >>JAK/STAT Signaling >>EGFRResearch Areas >>Cardiovascular DiseaseSignaling Pathways >>Anti-infection >>HCVResearch Areas >>InfectionSignaling Pathways >>Protein Tyrosine Kinase/RTK >>EGFRResearch Areas >>Metabolic Disease |
| Target | EGFR:3 nM (IC50) HCV EMCV |
| In Vitro | AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3]. |
| In Vivo | Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478[3]. |
| References | [1]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95. [2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580. [3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215. [4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6. |
Chemical & Physical Properties
| Density | 1.337g/cm3 |
|---|---|
| Boiling Point | 458.5ºC at 760mmHg |
| Molecular Formula | C16H15Cl2N3O2 |
| Molecular Weight | 352.215 |
| Flash Point | 231.1ºC |
| Exact Mass | 351.054138 |
| PSA | 56.27000 |
| LogP | 4.91900 |
| Vapour Pressure | 1.37E-08mmHg at 25°C |
| InChIKey | WDJDYIUSDDVWKB-UHFFFAOYSA-N |
| SMILES | COc1cc2ncnc(Nc3cccc(Cl)c3)c2cc1OC.Cl |
Safety Information
| HS Code | 2933990090 |
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Customs
| HS Code | 2933990090 |
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| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Synonyms
| N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine hydrochloride (1:1) |
| 6,7-Dimethoxy-4-[N-(3-chlorophenyl)amino]quinazoline hydrochloride |
| N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride (1:1) |
| 4-Quinazolinamine, N-(3-chlorophenyl)-6,7-dimethoxy-, hydrochloride (1:1) |
| N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine,hydrochloride |
| 6,7-Dimethoxy-4-[N-(3-chlorophenyl)amino]quinazolinehydrochloride |
